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Literature summary for 1.14.15.16 extracted from

  • Zhu, J.; Barycki, R.; Chiellini, G.; Deluca, H.F.
    Screening of selective inhibitors of 1alpha,25-dihydroxyvitamin D3 24-hydroxylase using recombinant human enzyme expressed in Escherichia coli (2010), Biochemistry, 49, 10403-10411.
    View publication on PubMed

Cloned(Commentary)

Cloned (Comment) Organism
expressed in Escherichia coli BL21-Gold(DE3) and Rosetta 2(DE3) cells Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
(1R,3S,5Z,7E,14x)-17-[(2R)-1-(1H-imidazol-1-yl)propan-2-yl]-2-methylidene-9,10-secoestra-5,7-diene-1,3-diol potent and selective CYP24A1 inhibitor Homo sapiens
(1R,3S,5Z,7E,14x)-17-[(2S)-7-cyclopropylheptan-2-yl]-2-methylidene-9,10-secoestra-5,7-diene-1,3-diol potent and selective CYP24A1 inhibitor Homo sapiens
(2R)-2-[(4E,7aR)-4-[(2Z)-2-[(5R)-5-hydroxy-2-methylidenecyclohexylidene]ethylidene]-7a-methyloctahydro-1H-inden-1-yl]propyl bromoacetate
-
Homo sapiens
(3R,5Z,7E,14x,17x,20S)-3-hydroxy-9,10-secochola-5,7,10-trien-24-yl 4-methylbenzenesulfonate
-
Homo sapiens
24-carboxyl-25-hydroxyvitamin D3
-
Homo sapiens
24-difluoro-1,25-dihydroxyvitamin D3
-
Homo sapiens
ketoconazole nonspecific CYP24A1 inhibitor Homo sapiens
liarozole nonspecific CYP24A1 inhibitor Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.00014
-
2-methylene-19-nor-(20S)-1,25-dihydroxyvitamin D3 in 20 mM Tris (pH 7.5), at 37°C Homo sapiens
0.00019
-
1alpha,25-dihydroxyvitamin D3 in 20 mM Tris (pH 7.5), at 37°C Homo sapiens
0.00033
-
25-hydroxyvitamin D3 in 20 mM Tris (pH 7.5), at 37°C Homo sapiens
0.00034
-
2-methylene-19-nor-(20R)-1,25-dihydroxyvitamin D3 in 20 mM Tris (pH 7.5), at 37°C Homo sapiens

Molecular Weight [Da]

Molecular Weight [Da] Molecular Weight Maximum [Da] Comment Organism
55000
-
about 55000 Da, SDS-PAGE Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Purification (Commentary)

Purification (Comment) Organism
Talon metal affinity column chromatography Homo sapiens

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
1alpha,25-dihydroxyvitamin D3 + NADPH + H+ + O2
-
Homo sapiens 1alpha,24R,25-trihydroxyvitamin D3 + NADP+ + H2O
-
?
2-methylene-19-nor-(20R)-1,25-dihydroxyvitamin D3 + NADPH + H+ + O2
-
Homo sapiens ? + NADP+ + H2O
-
?
2-methylene-19-nor-(20S)-1,25-dihydroxyvitamin D3 + NADPH + H+ + O2
-
Homo sapiens ? + NADP+ + H2O
-
?
25-hydroxyvitamin D3 + NADPH + H+ + O2
-
Homo sapiens 24R,25-dihydroxyvitamin D3 + NADP+ + H2O
-
?

Synonyms

Synonyms Comment Organism
1alpha,25-dihydroxyvitamin D3 24-hydroxylase
-
Homo sapiens
CYP24A1
-
Homo sapiens

Turnover Number [1/s]

Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
0.00025
-
2-methylene-19-nor-(20S)-1,25-dihydroxyvitamin D3 in 20 mM Tris (pH 7.5), at 37°C Homo sapiens
0.0017
-
2-methylene-19-nor-(20R)-1,25-dihydroxyvitamin D3 in 20 mM Tris (pH 7.5), at 37°C Homo sapiens
0.002
-
1alpha,25-dihydroxyvitamin D3 in 20 mM Tris (pH 7.5), at 37°C Homo sapiens
0.002
-
25-hydroxyvitamin D3 in 20 mM Tris (pH 7.5), at 37°C Homo sapiens

Cofactor

Cofactor Comment Organism Structure
heme CYP24A1 has a heme content of 77-85% Homo sapiens
NADPH
-
Homo sapiens

kcat/KM [mM/s]

kcat/KM Value [1/mMs-1] kcat/KM Value Maximum [1/mMs-1] Substrate Comment Organism Structure
1.8
-
2-methylene-19-nor-(20S)-1,25-dihydroxyvitamin D3 in 20 mM Tris (pH 7.5), at 37°C Homo sapiens
4.9
-
2-methylene-19-nor-(20R)-1,25-dihydroxyvitamin D3 in 20 mM Tris (pH 7.5), at 37°C Homo sapiens
6.1
-
25-hydroxyvitamin D3 in 20 mM Tris (pH 7.5), at 37°C Homo sapiens
10
-
1alpha,25-dihydroxyvitamin D3 in 20 mM Tris (pH 7.5), at 37°C Homo sapiens